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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2008-2-5
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pubmed:abstractText |
The introduction and the optimization of an alpha-amino substituent based on a series of alpha-hydroxy-beta-N-biaryl ether sulfonamide hydroxamates is described. The modification leads to a new series of MMP-2/MMP-9 inhibitors with enhanced inhibitory activities and improved ADME properties. An efficacy study on reducing the ischemia-induced brain edema in the rat transient middle cerebral artery occlusion (tMCAo) model is also demonstrated.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1140-5
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pubmed:meshHeading |
pubmed-meshheading:18083558-Amino Acids,
pubmed-meshheading:18083558-Animals,
pubmed-meshheading:18083558-Brain Edema,
pubmed-meshheading:18083558-Disease Models, Animal,
pubmed-meshheading:18083558-Drug Design,
pubmed-meshheading:18083558-Gelatinases,
pubmed-meshheading:18083558-Humans,
pubmed-meshheading:18083558-Hydroxamic Acids,
pubmed-meshheading:18083558-Matrix Metalloproteinase 2,
pubmed-meshheading:18083558-Matrix Metalloproteinase 9,
pubmed-meshheading:18083558-Microsomes, Liver,
pubmed-meshheading:18083558-Middle Cerebral Artery,
pubmed-meshheading:18083558-Molecular Structure,
pubmed-meshheading:18083558-Pyrazines,
pubmed-meshheading:18083558-Rats,
pubmed-meshheading:18083558-Stereoisomerism,
pubmed-meshheading:18083558-Structure-Activity Relationship,
pubmed-meshheading:18083558-Sulfonamides
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pubmed:year |
2008
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pubmed:articleTitle |
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents.
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pubmed:affiliation |
Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. syang9@prdus.jnj.com
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pubmed:publicationType |
Journal Article
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